CAS NO: | 1202055-32-0 |
包装 | 价格(元) |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | NMS-P715 is a selective, ATP-competitive inhibitor ofMPS1, with anIC50of 182 nM. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | NMS-P715 is a selective inhibitor of MPS1, with an IC50of 182 nM. NMS-P715 is highly specific for MPS1, with no other kinases inhibited below an IC50value of 5 μM and only 3 kinases inhibited below 10 μM (CK2, MELK, and NEK6). NMS-P715 promotes massive spindle assembly checkpoint (SAC) override with an EC50of 65 nM. NMS-P715 (1 μM) causes mitotic acceleration in U2OS cells overexpressing YFP-α-tubulin, induces aneuploidy and inhibits the proliferation of HCT116 cells. NMS-P715 (0.5, 1 μM) affects mitotic checkpoint complex (MCC) stability and cdc20 ubiquitylation[1]. NMS-P715 (1 μM) exhibits bypass of the spindle assembly checkpoint and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. NMS-P715 (0-25 μM) also selectively inhibits growth of PDAC cells[2]. | ||||||||||||||||
体内研究 (In Vivo) | NMS-P715 (10 mg/kg) exhibits an oral bioavailability of 37% and good pharmacokinetic properties in nude mice bearing subcutaneous implanted human tumor cell xenografts. NMS-P715 (90 mg/kg, p.o.) is well tolerated and cuases no signs of body weight loss or other overt toxicities in an A2780 ovary carcinoma xenograft model. NMS-P715 (100 mg/kg, p.o.) inhibits the tumor growth by appr 43% in the A375 melanoma xenograft model[1]. | ||||||||||||||||
分子量 | 676.73 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C35H39F3N8O3 | ||||||||||||||||
CAS 号 | 1202055-32-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 2 mg/mL(2.96 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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